公开(公告)号：US20090054494A1

公开(公告)日：2009-02-26

申请号：US12062764

申请日：2008-04-04

申请人： Stefanie KEIL ,  Hans MATTER ,  Karl SCHOENAFINGER ,  Mathias URMANN ,  Maike GLIEN ,  Wolfgang WENDLER ,  Hans-Ludwig SCHAEFER ,  Eugen FALK

发明人： Stefanie KEIL ,  Hans MATTER ,  Karl SCHOENAFINGER ,  Mathias URMANN ,  Maike GLIEN ,  Wolfgang WENDLER ,  Hans-Ludwig SCHAEFER ,  Eugen FALK

IPC分类号： A61K31/433 ,  C07D285/135 ,  A61K31/4439 ,  A61P3/00 ,  C07D417/12

CPC分类号： C07D417/12 ,  C07D285/135

摘要： The present invention comprises N-[1,3,4]-thiadiazol-2-yl-benzene sulfonamides, their physiologically acceptable salts and functional derivatives that exhibit peroxisome proliferator activated receptor (PPAR) PPARdelta and PPARgamma agonist activity. The structure of the compounds of the invention are defined by Formula I below, And the isomers thereof wherein the various substituents are defined herein, including their physiologically acceptable salts. Processes for the compounds preparation are also disclosed. The compounds are suitable for the treatment of fatty acid metabolism and glucose utilization disorders, disorders relating to insulin resistance are involved as well as demyelinating and other neurodegenerative disorders of the central and peripheral nervous system.

摘要翻译： 本发明包括显示过氧化物酶体增殖物激活受体（PPAR）PPARδ和PPARγ激动剂活性的N- [1,3,4] - 噻二唑-2-基 - 苯磺酰胺，其生理上可接受的盐和功能性衍生物。 本发明化合物的结构由下式I定义，其各种取代基在本文中定义的异构体，包括其生理上可接受的盐。 还公开了化合物制备的方法。 该化合物适用于治疗脂肪酸代谢和葡萄糖利用障碍，涉及胰岛素抵抗的疾病以及中枢和周围神经系统的脱髓鞘和其他神经变性疾病。

公开(公告)号：US20090012131A1

公开(公告)日：2009-01-08

申请号：US12062769

申请日：2008-04-04

申请人： Stefanie KEIL ,  Karl SCHOENAFINGER ,  Hans MATTER ,  Matthias URMANN ,  Maike GLIEN ,  Wolfgang WENDLER ,  Hans-Ludwig SCHAEFER ,  Eugen FALK

发明人： Stefanie KEIL ,  Karl SCHOENAFINGER ,  Hans MATTER ,  Matthias URMANN ,  Maike GLIEN ,  Wolfgang WENDLER ,  Hans-Ludwig SCHAEFER ,  Eugen FALK

IPC分类号： A61K31/433 ,  C07D285/135 ,  A61P3/00 ,  A61P3/10

CPC分类号： C07D285/135 ,  C07D417/12

摘要： The present invention comprises 4-Oxy-N-[1,3,4]-thiadiazol-2-yl-benzene sulfonamides, the derivatives thereof and salts thereof as well as processes for their preparation and methods for their use as pharmaceutical compositions. More specifically, the invention relates to 4-oxy-N-[1,3,4]-thiadiazol-2-yl-benzene sulfonamides and to their physiologically acceptable salts and physiologically functional derivatives that exhibit peroxisome proliferator activator receptor (PPAR) PPARalpha, PPARdelta and PPARgamma agonist activity. The compounds themselves are defined by the structure of the formula I, wherein the various unnamed substituents are defined herein. The compounds are suitable for the treatment of disorders of fatty acid metabolism and glucose utilization disorders as well as of disorders in which insulin resistance is involved as well as demyelinating and other neurodegenerative disorders of the central and peripheral nervous system.

摘要翻译： 本发明包括4-氧基-N- [1,3,4] - 噻二唑-2-基 - 苯磺酰胺及其衍生物及其盐，以及其制备方法及其用作药物组合物的方法。 更具体地，本发明涉及4-氧-N- [1,3,4] - 噻二唑-2-基 - 苯磺酰胺及其生理上可接受的盐和生理功能衍生物，其表现出过氧化物酶体增殖物激活受体（PPAR）PPARα， PPARδ和PPARgamma激动剂活性。 化合物本身由式I的结构定义，其中各种未命名的取代基在本文中定义。 该化合物适用于治疗脂肪酸代谢紊乱和葡萄糖利用障碍以及涉及胰岛素抵抗的疾病以及中枢和周围神经系统的脱髓鞘和其它神经变性疾病。

公开(公告)号：US20090298871A1

公开(公告)日：2009-12-03

申请号：US12480974

申请日：2009-06-09

申请人： Stefanie KEIL ,  Matthias URMANN ,  Karl SCHOENAFINGER ,  Wolfgang WENDLER ,  Maike GLIEN ,  Hans-Ludwig SCHAEFER ,  Eugen FALK

发明人： Stefanie KEIL ,  Matthias URMANN ,  Karl SCHOENAFINGER ,  Wolfgang WENDLER ,  Maike GLIEN ,  Hans-Ludwig SCHAEFER ,  Eugen FALK

IPC分类号： A61K31/4725 ,  C07D413/12 ,  A61K31/4245

CPC分类号： C07D413/12

摘要： The invention relates to sulfonyl-phenyl-oxadiazolones and to their physiologically acceptable salts and physiologically functional derivatives showing PPARdelta or PPARdelta and PPARgamma agonist activity.What are described are compounds of the formula I, in which the radicals are as defined, and their physiologically acceptable salts and processes for their preparations. The compounds are suitable for the treatment and/or prevention of disorders of fatty acid metabolism and glucose utilization disorders as well as of disorders in which insulin resistance is involved and demyelinating and other neurodegenerative disorders of the central and peripheral nervous system.

摘要翻译： 本发明涉及磺酰基 - 苯基 - 恶二唑酮及其生理上可接受的盐和生理功能衍生物，其显示PPARδ或PPARδ和PPARγ激动剂活性。 描述的是式I化合物，其中基团如所定义，以及它们的生理上可接受的盐及其制备方法。 该化合物适用于治疗和/或预防脂肪酸代谢紊乱和葡萄糖利用障碍以及其中涉及胰岛素抵抗和中枢神经和周围神经系统的脱髓鞘和其它神经变性疾病的疾病。

公开(公告)号：US20080171776A1

公开(公告)日：2008-07-17

申请号：US11949833

申请日：2007-12-04

申请人： Christian STAPPER ,  Heiner GLOMBIK ,  Eugen FALK ,  Stefanie KEIL ,  Hans-Ludwig SCHAEFER ,  Wolfgang WENDLER ,  Stephanie HACHTEL

发明人： Christian STAPPER ,  Heiner GLOMBIK ,  Eugen FALK ,  Stefanie KEIL ,  Hans-Ludwig SCHAEFER ,  Wolfgang WENDLER ,  Stephanie HACHTEL

IPC分类号： A61K31/421 ,  C07D263/32 ,  A61P3/00 ,  A61P3/10 ,  A61P3/08

CPC分类号： C07D263/32 ,  C07D413/04

摘要： The present invention comprises compounds and compositions for the treatment of metabolic disorders and more particularly, those insulin-related metabolic disorders of the blood such as hyperlipidemia, diabetes, insulin-resistance and the like comprising acetic acid derivatives with cyclohexylmethoxy substituents and their salts. Known as peroxisome proliferator-activated receptor (PPAR) agonists/antagonists, the invention relates to compounds of formula I wherein R1-R6 are further defined herein.

摘要翻译： 本发明包括用于治疗代谢紊乱的化合物和组合物，更具体地，涉及含有环己基甲氧基取代基的乙酸衍生物及其盐的血液中的这些与胰岛素有关的代谢性疾病如高脂血症，糖尿病，胰岛素抵抗等。 被称为过氧化物酶体增殖物激活受体（PPAR）激动剂/拮抗剂的本发明涉及式I化合物，其中R 1 -R 6在本文中进一步定义。

公开(公告)号：US20080015238A1

公开(公告)日：2008-01-17

申请号：US11839950

申请日：2007-08-16

申请人： Christian STAPPER ,  Stefanie KEIL ,  Heiner GLOMBIK ,  Eugen FALK ,  Jochen GOERLITZER ,  Dirk GRETZKE ,  Hans-Ludwig SCHAEFER ,  Wolfgang WENDLER

发明人： Christian STAPPER ,  Stefanie KEIL ,  Heiner GLOMBIK ,  Eugen FALK ,  Jochen GOERLITZER ,  Dirk GRETZKE ,  Hans-Ludwig SCHAEFER ,  Wolfgang WENDLER

IPC分类号： A61K31/421 ,  A61P3/00

CPC分类号： C07D263/32 ,  C07D413/02

摘要： Provided herein are methods for the treatment of metabolic diseases such as disorders of fatty acid metabolism and glucose utilization as well as disorders in which insulin resistance is involved, in a patient. comprising the administration of novel compounds of formula I below: in which the substituents are defined herein including their physiologically acceptable salts,

摘要翻译： 本文提供了用于治疗代谢疾病的方法，例如患者中脂肪酸代谢紊乱和葡萄糖利用以及涉及胰岛素抵抗的疾病。 包括施用以下式I的新化合物：其中取代基在本文中定义，包括其生理上可接受的盐，

公开(公告)号：US20090143473A1

公开(公告)日：2009-06-04

申请号：US12364703

申请日：2009-02-03

申请人： Hans Jochen LANG ,  Hans-Willi JANSEN ,  Jan-Robert SCHWARK ,  Heinz-Werner KLEEMANN ,  Oliver JUNG ,  Hans-Ludwig SCHAFER ,  Wolfgang LINZ ,  Werner KRAMER ,  Bernward SCHOLKENS ,  Eugen FALK

发明人： Hans Jochen LANG ,  Hans-Willi JANSEN ,  Jan-Robert SCHWARK ,  Heinz-Werner KLEEMANN ,  Oliver JUNG ,  Hans-Ludwig SCHAFER ,  Wolfgang LINZ ,  Werner KRAMER ,  Bernward SCHOLKENS ,  Eugen FALK

IPC分类号： A61K31/165 ,  A61P7/00

CPC分类号： A61K31/00 ,  A61K31/155 ,  A61K31/166 ,  A61K31/22 ,  A61K31/365 ,  A61K2300/00

摘要： Use of inhibitors of the cellular Na+/H+ exchanger (NHE) for the production of a medicament for the normalization of serum lipids.The active compounds identified as inhibitors of the cellular Na+/H+ exchanger (NHE) are used for the production of a medicament for the normalization of serum lipids.They are used for the production of a medicament for lowering the blood lipid level and illnesses caused thereby, as well as the endothelial dysfunction syndrome and illness caused thereby.

摘要翻译： 使用细胞Na + / H +交换剂（NHE）的抑制剂来制备用于血清脂质标准化的药物。 鉴定为细胞Na + / H +交换体（NHE）的抑制剂的活性化合物用于制备用于血清脂质标准化的药物。 它们用于制备用于降低由此引起的血脂水平和疾病以及由此引起的内皮功能障碍综合征和疾病的药物。